1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Dopamine Receptor
    5-HT Receptor
    Histamine Receptor
  3. UNC9994

UNC9994 

Cat. No.: HY-117829
Handling Instructions

UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity.

For research use only. We do not sell to patients.

UNC9994 Chemical Structure

UNC9994 Chemical Structure

CAS No. : 1354030-51-5

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Description

UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity[1].

IC50 & Target[1]

D2 Receptor

79 nM (Ki)

D3 Receptor

17 nM (Ki)

D4 Receptor

138 nM (Ki)

5-HT2A Receptor

140 nM (Ki)

5-HT2B Receptor

25 nM (Ki)

5-HT2C Receptor

512 nM (Ki)

5-HT1F Receptor

26 nM (Ki)

H1-histamine receptor

2.4 nM (Ki)

H1-histamine receptor

79 (pA2)

In Vitro

UNC9994 displays a lower binding affinity (Ki=79 nM) to D2R than UNC9975, UNC0006, and aripiprazole. At serotonin (as known as 5-HT) receptors, UNC9994 displays moderate to high binding affinities (Ki=25-512 nM) for 5HT2A, 5HT2B, 5HT2C, and 5HT1A, but is significantly less potent in functional assays (Ca2+ mobilization FLIPR or cAMP biosensor). UNC9994 is an antagonist at 5HT2A and 5HT2B and agonists at 5HT2C and 5HT1A. UNC9994 has relatively high affinities to H1-histamine receptor (Ki=2.4 nM) but is less potent antagonists in H1 functional assays[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The antipsychotic-like activity displayed by UNC9994 (2 mg/kg; i.p.) in wild-type mice is completely abolished in β-arrestin-2 knockout mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J wild-type and β-arrestin-2 knockout mice (phencyclidine-induced hyperlocomotion)[1]
Dosage: 2 mg/kg
Administration: I.p. followed 30 min later with 6 mg/kg phencyclidine
Result: Markedly inhibited PCP-induced hyperlocomotion in wild-type mice. This significant antipsychotic-like activity of UNC9994 was completely abolished in β-arrestin-2 knockout mice.
Molecular Weight

421.38

Formula

C₂₁H₂₂Cl₂N₂OS

CAS No.
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UNC9994
Cat. No.:
HY-117829
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